Detalhe da pesquisa
1.
Discovery of structural diverse reversible BTK inhibitors utilized to develop a novel in vivo CD69 and CD86 PK/PD mouse model.
Bioorg Med Chem Lett
; 80: 129108, 2023 01 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-36538993
2.
Mechanisms of Regulation and Diverse Activities of Tau-Tubulin Kinase (TTBK) Isoforms.
Cell Mol Neurobiol
; 41(4): 669-685, 2021 May.
Artigo
em Inglês
| MEDLINE | ID: mdl-32424773
3.
Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.
Bioorg Med Chem
; 44: 116275, 2021 08 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-34314938
4.
Design, synthesis and identification of novel, orally bioavailable non-covalent Nrf2 activators.
Bioorg Med Chem Lett
; 30(4): 126852, 2020 02 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31898999
5.
Optimization of novel reversible Bruton's tyrosine kinase inhibitors identified using Tethering-fragment-based screens.
Bioorg Med Chem
; 27(13): 2905-2913, 2019 07 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-31138459
6.
Investigating small molecules to inhibit germinal center kinase-like kinase (GLK/MAP4K3) upstream of PKCθ phosphorylation: Potential therapy to modulate T cell dependent immunity.
Bioorg Med Chem Lett
; 28(10): 1964-1971, 2018 06 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-29636220
7.
Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.
J Biol Chem
; 290(8): 4573-4589, 2015 Feb 20.
Artigo
em Inglês
| MEDLINE | ID: mdl-25552479
8.
Structural determinant for inducing RORgamma specific inverse agonism triggered by a synthetic benzoxazinone ligand.
BMC Struct Biol
; 16(1): 7, 2016 06 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27246200
9.
Discovery of biaryls as RORγ inverse agonists by using structure-based design.
Bioorg Med Chem Lett
; 26(10): 2459-2463, 2016 05 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27080181
10.
Discovery of novel pyrazole-containing benzamides as potent RORγ inverse agonists.
Bioorg Med Chem Lett
; 25(15): 2985-90, 2015 Aug 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26048789
11.
Discovery of biaryl carboxylamides as potent RORγ inverse agonists.
Bioorg Med Chem Lett
; 25(15): 2991-7, 2015 Aug 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26048806
12.
Discovery of Potent Isoindolinone Inhibitors that Target an Active Conformation of PARP1 Using DNA-Encoded Libraries.
ChemMedChem
; 19(11): e202400093, 2024 Jun 03.
Artigo
em Inglês
| MEDLINE | ID: mdl-38482564
13.
Small molecules inhibit the interaction of Nrf2 and the Keap1 Kelch domain through a non-covalent mechanism.
Bioorg Med Chem
; 21(14): 4011-9, 2013 Jul 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23647822
14.
Elucidation of the GSK3α Structure Informs the Design of Novel, Paralog-Selective Inhibitors.
ACS Chem Neurosci
; 14(6): 1080-1094, 2023 03 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-36812145
15.
Structure-based design of 2,6,7-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines as Aurora kinases inhibitors.
Bioorg Med Chem Lett
; 22(12): 4033-7, 2012 Jun 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-22607669
16.
Discovery of Potent Selective Nonzinc Binding Autotaxin Inhibitor BIO-32546.
ACS Med Chem Lett
; 12(7): 1124-1129, 2021 Jul 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-34267882
17.
Discovery of Potent, Selective, and Brain-Penetrant Apoptosis Signal-Regulating Kinase 1 (ASK1) Inhibitors that Modulate Brain Inflammation In Vivo.
J Med Chem
; 64(20): 15402-15419, 2021 10 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-34653340
18.
Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
J Med Chem
; 64(9): 6358-6380, 2021 05 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-33944571
19.
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.
Bioorg Med Chem Lett
; 20(1): 330-3, 2010 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19919896
20.
The crystal structure of the catalytic domain of tau tubulin kinase 2 in complex with a small-molecule inhibitor.
Acta Crystallogr F Struct Biol Commun
; 76(Pt 3): 103-108, 2020 Mar 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-32133995